Olanzapine

Olanzapine Elisa Q. 2020-07-11T20:31:51+08:00

Olanzapine

Olanzapine是一种高亲和力的5-HT2 5-羟色胺和多巴胺D2受体拮抗剂。

中文名：奥氮平

英文名：Olanzapine;LY170053

CAS 号： 132539-06-1

分子式：C₁₇H₂₀N₄S

分子量：312.432

纯度：>98.0%

Description	Olanzapine (LY170053) is a selective monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
Target	5-HT2;D2 receptor
In Vitro	Olanzapine binds weakly to GABAA, Benzodiazepine (BZD), and β-adrenergic receptors (Ki>10 μM) [1][2]. Olanzapine induces autophagy in human SH-SY5Y neuronal cell line[3]. Olanzapine (1-100 μM for 144 h under serum starvation) results in a marked anti-proliferative effect in glioblastoma cell lines as well as glioma stem-like cells[4]. Olanzapine also enhances Temozolomide’s anti-tumor activity in glioblastoma cell lines[4]. Olanzapine induces apoptosis and necrosis in glioblastoma cell lines[4].
In Vivo	Olanzapine (0.75, 1.5 and 3 mg/kg) evaluates body weight and periuterine fat mass, as well as insulin, non-esterified fatty acids, triglycerides, and glucose levels in mice[5]
References	[1]. APPROVED AGREED-UPON LABELING. [2]. Olanzapine for Injection, powder, for solution for intramuscular use. [3]. Vucicevic L, et al. Autophagy inhibition uncovers the neurotoxic action of the antipsychotic drug olanzapine. Autophagy. 2014;10(12):2362-78. [4]. Karpel-Massler G, et al. Olanzapine inhibits proliferation, migration and anchorage-independent growth in human glioblastoma cell lines and enhances temozolomide's antiproliferative effect. J Neurooncol. 2015 Mar;122(1):21-33. [5]. Coccurello R, et al. Chronic administration of olanzapine induces metabolic and food intake alterations: a mousemodel of the atypical antipsychotic-associated adverse effects. Psychopharmacology (Berl). 2006 Jul;186(4):561-71.

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